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Chronic caffeine alters the density of adenosine,adrenergic, cholinergic,GABA, and serotonin receptors and calcium channels in mouse brain
Authors:Dan Shi  Olga Nikodijević  Kenneth A Jacobson  John W Daly
Institution:1. Laboratory of Bioorganic Chemistry, National Institute of Diabetes and Digestive and Kidney Diseases, National Institutes of Health, 20892, Bethesda, MD, USA
Abstract:
1.  Chronic ingestion of caffeine by male NIH strain mice alters the density of a variety of central receptors.
2.  The density of cortical A1 adenosine receptors is increased by 20%, while the density of striatal A2A adenosine receptors is unaltered.
3.  The densities of corticalbeta 1 and cerebellarbeta 2 adrenergic receptors are reduced byca. 25%, while the densities of corticalagr 1 andagr 2 adrenergic receptors are not significantly altered. Densities of striatal D1 and D2 dopaminergic receptors are unaltered. The densities of cortical 5 HT1 and 5 HT2 serotonergic receptors are increased by 26–30%. Densities of cortical muscarinic and nicotinic receptors are increased by 40–50%. The density of cortical benzodiazepine-binding sites associated with GABAA receptors is increased by 65%, and the affinity appears slightly decreased. The density of cortical MK-801 sites associated with NMDA-glutaminergic receptors appear unaltered.
4.  The density of cortical nitrendipine-binding sites associated with calcium channels is increased by 18%.
5.  The results indicate that chronic ingestion of caffeine equivalent to about 100 mg/kg/day in mice causes a wide range of biochemical alterations in the central nervous system.
Keywords:caffeine  adenosine receptors  adrenergic receptors  cholinergic receptors  serotonin receptors  GABA receptors  calcium channels  dopamine receptors  NMDA receptors
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